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安哥拉紫玉盘作为一种有潜力的HIV-1逆转录酶相关RNA依赖性DNA聚合酶和核糖核酸酶H功能抑制剂的来源。

Uvaria angolensis as a promising source of inhibitors of HIV-1 RT-associated RNA-dependent DNA polymerase and RNase H functions.

作者信息

Ngoutane Mfopa Alvine, Corona Angela, Eloh Kodjo, Tramontano Enzo, Frau Aldo, Boyom Fabrice Fekam, Caboni Pierluigi, Tocco Graziella

机构信息

a Laboratory for Phytobiochemistry and Medicinal Plants Studies, Faculty of Science , University of Yaoundé I , Yaoundé , Cameroon.

b Department of Life and Environmental Sciences , University of Cagliari , Cagliari , Italy.

出版信息

Nat Prod Res. 2018 Mar;32(6):640-647. doi: 10.1080/14786419.2017.1332615. Epub 2017 May 25.

Abstract

Reverse transcriptase (RT)-associated DNA polymerase (RDDP) and ribonucleaser H (RNase H) functions are both essential for HIV-1 genome replication, and the identification of new inhibitors to block both of them is a goal actively pursued by the scientific community. In this field, natural extracts have shown a great potential as source of new antivirals. In the present work, we investigated the effect of Uvaria angolensis extracts on the HIV-1 reverse transcriptase-associated DNA polymerase and ribonuclease H activities. The U. angolensis stem bark methanol extract inhibit both HIV-1 RNase H function and RDDP activity with IC values of 1.0 ± 0.2 and 0.62 ± 0.15 μg/mL, respectively and, after been fractionated with different solvents, its solid residue showed an IC of 0.10 ± 0.03 and of 0.23 ± 0.04 μg/mL against RNase H and RDDP, respectively, hence laying the bases for further studies for identification of single active components.

摘要

逆转录酶(RT)相关的DNA聚合酶(RDDP)和核糖核酸酶H(RNase H)的功能对于HIV-1基因组复制均至关重要,鉴定能够同时阻断这两种酶的新型抑制剂是科学界积极追求的目标。在该领域,天然提取物已显示出作为新型抗病毒药物来源的巨大潜力。在本研究中,我们研究了安哥拉紫玉盘提取物对HIV-1逆转录酶相关DNA聚合酶和核糖核酸酶H活性的影响。安哥拉紫玉盘茎皮甲醇提取物对HIV-1 RNase H功能和RDDP活性均有抑制作用,其IC值分别为1.0±0.2和0.62±0.15μg/mL,在用不同溶剂分级分离后,其固体残渣对RNase H和RDDP的IC值分别为0.10±0.03和0.23±0.04μg/mL,从而为进一步研究鉴定单一活性成分奠定了基础。

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